Two step one-pot synthesis of 7-azaindole linked 1,2,3-triazole hybrids: In-vitro and in-silico antimicrobial evaluation.
ChemMedChem
; : e202400451, 2024 Aug 18.
Article
in En
| MEDLINE
| ID: mdl-39155530
ABSTRACT
Herein, we report design, synthesis and characterization of a new library of 7-azaindole N-ethyl linked 1,2,3-triazoles containing ethylene as a spacer unit, and evaluation of all the synthesized compounds for their antimicrobial properties. Antibacterial potential was checked against two Gram positive (B. subtilis and S. aureus) and two Gram negative (E. coli and P. aeruginosa) bacterial strains while antifungal potential was assayed against two fungal strains (C. albicans and A. niger). All the tested compounds showed satisfactory antibacterial potency in comparison to reference drug ciprofloxacin with MIC values ranging from 0.0108 to 0.0432 µmol/mL. Interestingly, except two, all the target compounds showed better antifungal property as compared to the reference drug fluconazole with MIC values less than 0.0408 µmol/mL. One of the compounds exhibited two-fold better antifungal potential in comparison to fluconazole. Furthermore, in-silico ADMET and DFT studies reported drug likeness behavior and chemical reactivity parameters, respectively. The cytotoxicity results on substrate azide 3 and most potent 1,2,3-triazoles (5d and 5l) were found to be non-toxic.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
ChemMedChem
Year:
2024
Document type:
Article